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CRA-026440

CRA-026440
CRA-026440(PCI-34051) is a highly potent HDAC inhibitor with inhibitory effects on HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC10 with Ki values of 4,14,11,15,7 and 20 nM, respectively. CRA-026440 has anti-tumor and anti-angiogenic activity and can be used to study colon cancer.
Catalog No. T10883Cas No. 847460-34-8
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Purity:96.42%
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CRA-026440

Catalog No. T10883Cas No. 847460-34-8
CRA-026440(PCI-34051) is a highly potent HDAC inhibitor with inhibitory effects on HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC10 with Ki values of 4,14,11,15,7 and 20 nM, respectively. CRA-026440 has anti-tumor and anti-angiogenic activity and can be used to study colon cancer.
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1 mg$700In Stock
5 mg$1,800In Stock
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Product Introduction

Bioactivity
Description
CRA-026440(PCI-34051) is a highly potent HDAC inhibitor with inhibitory effects on HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC10 with Ki values of 4,14,11,15,7 and 20 nM, respectively. CRA-026440 has anti-tumor and anti-angiogenic activity and can be used to study colon cancer.
Targets&IC50
HDAC6:15 nM (ki), HDAC1:4 nM (ki), HDAC2:14 nM (ki), HDAC10:20 nM (Ki), HDAC3:11 nM (ki), HDAC8:7 nM (ki)
In vitro
CRA-026440 exhibits anti-proliferative effects on HUVEC endothelial cells with a GI50 value of 1.41 μM[1].
In tumor cells, treatment with CRA-026440 (0.1-10 μM; 18 hours) leads to the accumulation of acetylated histones and acetylated microtubule proteins, thereby inhibiting tumor cell growth and inducing apoptosis[1].
CRA-026440 (0.1-10 μM; 5 days) inhibits ex vivo angiogenesis in a dose-dependent manner[1].
In vivo
Administered intravenously at a dose of 100 mg/kg daily for three consecutive days, CRA-026440 significantly reduces tumor growth in mice bearing HCT116 or U937 human tumor xenografts[1].
AliasPCI-34051
Chemical Properties
Molecular Weight420.46
FormulaC23H24N4O4
Cas No.847460-34-8
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 90 mg/mL (214.05 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3783 mL11.8917 mL23.7835 mL118.9174 mL
5 mM0.4757 mL2.3783 mL4.7567 mL23.7835 mL
10 mM0.2378 mL1.1892 mL2.3783 mL11.8917 mL
20 mM0.1189 mL0.5946 mL1.1892 mL5.9459 mL
50 mM0.0476 mL0.2378 mL0.4757 mL2.3783 mL
100 mM0.0238 mL0.1189 mL0.2378 mL1.1892 mL

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